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Tablet Formulations of Polymeric Electrospun Fibers for the Controlled Release of Drugs with pH-Dependent Solubility
A challenge in the pharmaceutical sector is the development of controlled release dosage forms for oral administration of poorly soluble drugs, in particular, drugs characterized by pH-dependent solubility through the gastrointestinal tract, which itself shows wide variability in terms of environmen...
Autores principales: | , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2022
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9142934/ https://www.ncbi.nlm.nih.gov/pubmed/35632009 http://dx.doi.org/10.3390/polym14102127 |
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author | Friuli, Valeria Pisani, Silvia Conti, Bice Bruni, Giovanna Maggi, Lauretta |
author_facet | Friuli, Valeria Pisani, Silvia Conti, Bice Bruni, Giovanna Maggi, Lauretta |
author_sort | Friuli, Valeria |
collection | PubMed |
description | A challenge in the pharmaceutical sector is the development of controlled release dosage forms for oral administration of poorly soluble drugs, in particular, drugs characterized by pH-dependent solubility through the gastrointestinal tract, which itself shows wide variability in terms of environmental pHs. The best approach is to increase the dissolution rate of the drugs at the different pHs and only then modify its release behavior from the pharmaceutical form. This work aims to demonstrate the ability of properly designed polymeric nanofibers in enhancing the release rate of model drugs with different pH-dependent solubility in the different physiological pHs of the gastrointestinal tract. Polymeric nanofibers loaded with meloxicam and carvedilol were prepared using the electrospinning technique and were then included in properly designed tablet formulations to obtain fast or sustained release dosage forms. The nanofibers and the tablets were characterized for their morphological, physico-chemical and dissolution properties. The tablets are able to deliver the dose according to the expected release behavior, and zero-order, first-order, Higuchi, Korsmeyer–Peppas and Hixon–Crowell kinetics models were used to analyze the prevailing release mechanism of the tablets. This study shows that the electrospun fibers can be advantageously included in oral dosage forms to improve their release performances. |
format | Online Article Text |
id | pubmed-9142934 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-91429342022-05-29 Tablet Formulations of Polymeric Electrospun Fibers for the Controlled Release of Drugs with pH-Dependent Solubility Friuli, Valeria Pisani, Silvia Conti, Bice Bruni, Giovanna Maggi, Lauretta Polymers (Basel) Article A challenge in the pharmaceutical sector is the development of controlled release dosage forms for oral administration of poorly soluble drugs, in particular, drugs characterized by pH-dependent solubility through the gastrointestinal tract, which itself shows wide variability in terms of environmental pHs. The best approach is to increase the dissolution rate of the drugs at the different pHs and only then modify its release behavior from the pharmaceutical form. This work aims to demonstrate the ability of properly designed polymeric nanofibers in enhancing the release rate of model drugs with different pH-dependent solubility in the different physiological pHs of the gastrointestinal tract. Polymeric nanofibers loaded with meloxicam and carvedilol were prepared using the electrospinning technique and were then included in properly designed tablet formulations to obtain fast or sustained release dosage forms. The nanofibers and the tablets were characterized for their morphological, physico-chemical and dissolution properties. The tablets are able to deliver the dose according to the expected release behavior, and zero-order, first-order, Higuchi, Korsmeyer–Peppas and Hixon–Crowell kinetics models were used to analyze the prevailing release mechanism of the tablets. This study shows that the electrospun fibers can be advantageously included in oral dosage forms to improve their release performances. MDPI 2022-05-23 /pmc/articles/PMC9142934/ /pubmed/35632009 http://dx.doi.org/10.3390/polym14102127 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Friuli, Valeria Pisani, Silvia Conti, Bice Bruni, Giovanna Maggi, Lauretta Tablet Formulations of Polymeric Electrospun Fibers for the Controlled Release of Drugs with pH-Dependent Solubility |
title | Tablet Formulations of Polymeric Electrospun Fibers for the Controlled Release of Drugs with pH-Dependent Solubility |
title_full | Tablet Formulations of Polymeric Electrospun Fibers for the Controlled Release of Drugs with pH-Dependent Solubility |
title_fullStr | Tablet Formulations of Polymeric Electrospun Fibers for the Controlled Release of Drugs with pH-Dependent Solubility |
title_full_unstemmed | Tablet Formulations of Polymeric Electrospun Fibers for the Controlled Release of Drugs with pH-Dependent Solubility |
title_short | Tablet Formulations of Polymeric Electrospun Fibers for the Controlled Release of Drugs with pH-Dependent Solubility |
title_sort | tablet formulations of polymeric electrospun fibers for the controlled release of drugs with ph-dependent solubility |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9142934/ https://www.ncbi.nlm.nih.gov/pubmed/35632009 http://dx.doi.org/10.3390/polym14102127 |
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